7393. Piboserod
Nomenclature
CAS number: 152811-62-6
N-[(1-Butyl-4-piperidinyl)methyl]-3,4-dihydro-2H-[1,3]oxazino[3,2-a]indole-10-carboxamide; SB-207266. C22H31N3O2; mol wt 369.50.
C 71.51%, H 8.46%, N 11.37%, O 8.66%.
Description and references
Selective 5-HT4 receptor antagonist. Prepn: L. M. Gaster, P. A. Wyman, WO 9318036; eidem, US 5852014 (1993, 1998 both to SKB). In vitro and in vivo studies of bioavailability, pharmacokinetics, and duration: K. A. Wardle et al., Br. J. Pharmacol. 118, 665 (1996). Effect on gastrointestinal function: G. J. Sanger et al., Neurogastroenterol. Motil. 10, 271 (1998); idem et al., Br. J. Pharmacol. 130, 706 (2000). Clinical evaluation in irritable bowel syndrome: L. A. Houghton et al., Aliment. Pharmacol. Ther. 13, 1437 (1999).
Properties
White solid from ether, mp 110-113°.Derivative
Hydrochloride.Nomenclature
CAS number: 178273-87-5
SB-207266A. C22H31N3O2.HCl; mol wt 405.96.
C 65.09%, H 7.95%, N 10.35%, O 7.88%, Cl 8.73%.
Properties
White crystals from ETOH/petrol, mp 254-256° (dec).Therapeutic Category
Gastroprokinetic
Keywords
Gastroprokinetic; Serotonin Receptor Antagonist